Investigation of 8-methoxy-3-(4-nitrobenzoyl)-6-propyl-2H-chromen-2-one as a promising coumarin compound for the development of a new and orally effective antileishmanial agent.

This study investigated the in vitro and in vivo leishmanicidal activity of synthetic coumarin compounds (C1-C5) in parasites Leishmania (L.) amazonensis and L. (L.) infantum chagasi. The cytotoxicity of these compounds in mammalian cells and their influence on production of reactive oxygen species was also investigated. In vitro assays showed that 8-methoxy-3-(4-nitrobenzoyl)-6-propyl-2H-chromen-2-one (C4) was as active as AMP B mainly in the amastigote form (p 
Source: Molecular Biology Reports - Category: Molecular Biology Authors: Tags: Mol Biol Rep Source Type: research

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Abstract The protozoan parasite Leishmania spp. causes leishmaniases, a group of diseases creating serious health problems in many parts of the world with significant resistance to existing drugs. Insect derived antimicrobial peptides are promising alternatives to conventional drugs against several human disease-causing pathogens because they do not generate resistance. Halictine-2, a novel antimicrobial peptide from the venom of eusocial honeybee, Halictus sexcinctus showed significant anti-leishmanial activity in vitro, towards two life forms of the dimorphic parasite, the free-swimming infective metacyclic prom...
Source: Experimental Parasitology - Category: Parasitology Authors: Tags: Exp Parasitol Source Type: research
ConclusionsThis study detected the blood sources andLeishmania parasites infection of sand flies by molecular methods in the extension region of Loess Plateau, China. A high epidemic risk of leishmaniasis is currently indicated by the results as the infection ofLeishmania in sand flies, the extensive blood sources of sand flies including humans, and positive antibody ofLeishmania in local dog sera. Given the recent increase of VL cases, asymptomatic patients, dogs and other potential infected animals should be screened and treated. Furthermore, the density of sand flies needs to be controlled and personal protection should be strengthened.
Source: Infectious Diseases of Poverty - Category: Infectious Diseases Source Type: research
by Nathalia Pinho, Jacek R. Wi śniewski, Geovane Dias-Lopes, Leonardo Saboia-Vahia, Ana Cristina Souza Bombaça, Camila Mesquita-Rodrigues, Rubem Menna-Barreto, Elisa Cupolillo, Jose Batista de Jesus, Gabriel Padrón, Patricia CuervoLeishmania species are responsible for a broad spectrum of diseases, denominated Leishmaniasis, affecting over 12 million people worldwide. During the last decade, there have been impressive efforts for sequencing the genome of most of the pathogenicLeishmania spp. as well as hundreds of strains, but large-scale proteomics analyses did not follow these achievements and theLeishmani...
Source: PLoS Neglected Tropical Diseases - Category: Tropical Medicine Authors: Source Type: research
In this study we analyzed the substance A11K3, a dibenzylideneacetone (DBA). DBAs have an acyclic dienone attached to aryl groups in both β-positions and studies have shown that they have biological activity against tumors cells, bacteria, and protozoa such as T. cruzi and Leishmania spp. Here we show that A11K3 is active against all three T. cruzi evolutionary forms: the epimastigote (IC50 = 3.3 ± 0.8), the trypomastigote (EC50 = 24 ± 4.3) and the intracellular amastigote (IC50 = 9.3 ± 0.5 µM). A cytotoxicity assay in LLCMK2 cells showed a CC50 of 239.2 ± 15.7 µM gi...
Source: Acta Tropica - Category: Infectious Diseases Authors: Tags: Acta Trop Source Type: research
ConclusionWith regard to the supportive role of bax in apoptosis and the preventive role of Leishmania in its function, it seems that expression of bax gene in parasite by technologies like transgenic or down regulating of anti-apoptotic molecule Bcl-2 by miRNA could be prompted the apoptosis process of infected-macrophages and inhibited extensive spread of Leishmania and the resulting lesions.
Source: Microbial Pathogenesis - Category: Infectious Diseases Source Type: research
Abstract Leishmaniasis, caused by the intracellular protozoan parasite Leishmania, remains an important neglected tropical infectious disease. Infection may be lethal if untreated. Currently, the available drugs for the disease are limited by high toxicity and drug resistance. There is an urgent need to develop novel anti-leishmanial strategies. Antimicrobial peptides (AMPs) have been described as the first-line immune defense against pathogenic microbes and are being developed as emerging anti-parasitic therapies. In the present study, we showed the anti-leishmanial activity of the synthetic 4-amino acid peptide ...
Source: Acta Biochimica et Biophysica Sinica - Category: Biochemistry Authors: Tags: Acta Biochim Biophys Sin (Shanghai) Source Type: research
The molecular mechanisms underlying biological differences between two Leishmania species that cause cutaneous disease, L. major and L. amazonensis, are poorly understood. In L. amazonensis, reactive oxygen species (ROS) signaling drives differentiation of nonvirulent promastigotes into forms capable of infecting host macrophages. Tight spatial and temporal regulation of H2O2 is key to this signaling mechanism, suggesting a role for ascorbate-dependent peroxidase (APX), which degrades mitochondrial H2O2. Earlier studies showed that APX-null L. major parasites are viable, accumulate higher levels of H2O2, generate a greater...
Source: Infection and Immunity - Category: Infectious Diseases Authors: Tags: Fungal and Parasitic Infections Source Type: research
Publication date: Available online 15 November 2019Source: Chemico-Biological InteractionsAuthor(s): Paula Roberta da Silva, Jamerson Ferreira de Oliveira, Anekécia Lauro da Silva, Camila Marques Queiroz, Ana Paula Sampaio Feitosa, Denise Maria Figueiredo Araújo Duarte, Aline Caroline da Silva, Maria Carolina Accioly Brelaz de Castro, Valéria Rêgo Alves Pereira, Rosali Maria Ferreira da Silva, Luiz Carlos Alves, Fábio André Brayner dos Santos, Maria do Carmo Alves de LimaAbstractParasitic diseases still represent serious public health problems, since the high and steady emergence of...
Source: Chemico Biological Interactions - Category: Biochemistry Source Type: research
In conclusion, the L. infantum death may be ascribed by the subcellular alterations followed by a pronounced decrease in the mitochondrial membrane potential, indicating dysfunction in the respiratory chain upon H1-antihistamine treatment. These H1-antihistamines could be used to explore new routes of cellular death in the parasite and the determination of the targets at a molecular level, would contribute to understanding the potential of these drugs as antileishmanial. PMID: 31002807 [PubMed - as supplied by publisher]
Source: Acta Tropica - Category: Infectious Diseases Authors: Tags: Acta Trop Source Type: research
In this study we found blocking autophagy led to increased CP growth in both macrophages and mouse embryonic fibroblasts. In vivo, loss of the autophagy elongation component ATG16L1 specifically in myeloid cells led to increased mortality in response to CP infection, characterized by greater numbers of neutrophils and dendritic cells, but no change in the CP burden in the lungs. This was accompanied by an increase in inflammasome-active macrophages and IL-1β production. While induction of autophagy in macrophages led to reduced CP growth in vitro, in vivo treatment with rapamycin led to increased mortality of infected...
Source: Frontiers in Immunology - Category: Allergy & Immunology Source Type: research
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